Literature DB >> 17113292

Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.

Glenn Noronha1, Kathy Barrett, Antonio Boccia, Tessa Brodhag, Jianguo Cao, Chun P Chow, Elena Dneprovskaia, John Doukas, Richard Fine, Xianchang Gong, Colleen Gritzen, Hong Gu, Ehab Hanna, John D Hood, Steven Hu, Xinshan Kang, Jann Key, Boris Klebansky, Ahmed Kousba, Ge Li, Dan Lohse, Chi Ching Mak, Andrew McPherson, Moorthy S S Palanki, Ved P Pathak, Joel Renick, Feng Shi, Richard Soll, Ute Splittgerber, Silva Stoughton, Suhan Tang, Shiyin Yee, Binqi Zeng, Ningning Zhao, Hong Zhu.   

Abstract

We describe the identification of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine (3), a potent, orally active Src inhibitor with desirable PK properties, demonstrated activity in human tumor cell lines and in animal models of tumor growth.

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Year:  2006        PMID: 17113292     DOI: 10.1016/j.bmcl.2006.11.006

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

1.  Retinal vascular permeability suppression by topical application of a novel VEGFR2/Src kinase inhibitor in mice and rabbits.

Authors:  Lea Scheppke; Edith Aguilar; Ray F Gariano; Ruth Jacobson; John Hood; John Doukas; Jon Cao; Glenn Noronha; Shiyin Yee; Sara Weis; Michael B Martin; Richard Soll; David A Cheresh; Martin Friedlander
Journal:  J Clin Invest       Date:  2008-06       Impact factor: 14.808

Review 2.  Fyn: a novel molecular target in cancer.

Authors:  Yoshihito D Saito; Ana R Jensen; Ravi Salgia; Edwin M Posadas
Journal:  Cancer       Date:  2010-04-01       Impact factor: 6.860

3.  An anti-inflammatory role of VEGFR2/Src kinase inhibitor in herpes simplex virus 1-induced immunopathology.

Authors:  Shalini Sharma; Sachin Mulik; Naveen Kumar; Amol Suryawanshi; Barry T Rouse
Journal:  J Virol       Date:  2011-04-06       Impact factor: 5.103

4.  In silico investigation of potential SRC kinase ligands from traditional Chinese medicine.

Authors:  Weng Ieong Tou; Calvin Yu-Chian Chen
Journal:  PLoS One       Date:  2012-03-21       Impact factor: 3.240

5.  Fyn expression is associated with the response of patients with locally advanced uterine cervical squamous cell carcinoma to neoadjuvant chemotherapy.

Authors:  Shigenori Nanno; Takeshi Fukuda; Takuya Noda; Eijiro Uchikura; Yuichiro Awazu; Kenji Imai; Makoto Yamauchi; Tomoyo Yasui; Toshiyuki Sumi
Journal:  Mol Clin Oncol       Date:  2022-08-11

6.  Development and experimental test of support vector machines virtual screening method for searching Src inhibitors from large compound libraries.

Authors:  Bucong Han; Xiaohua Ma; Ruiying Zhao; Jingxian Zhang; Xiaona Wei; Xianghui Liu; Xin Liu; Cunlong Zhang; Chunyan Tan; Yuyang Jiang; Yuzong Chen
Journal:  Chem Cent J       Date:  2012-11-23       Impact factor: 4.215

7.  Kinase inhibitors for the treatment of inflammatory and autoimmune disorders.

Authors:  Shripad S Bhagwat
Journal:  Purinergic Signal       Date:  2008-06-21       Impact factor: 3.765

8.  Post-translational regulation of COX2 activity by FYN in prostate cancer cells.

Authors:  Anna Alexanian; Bradley Miller; Marla Chesnik; Shama Mirza; Andrey Sorokin
Journal:  Oncotarget       Date:  2014-06-30
  8 in total

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